GW311616 hydrochloride (Synonyms: GW311616A) |
カタログ番号GC13851
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GW-311616 は、経口で生体利用可能な強力な長期選択的ヒト好中球エラスターゼ (HNE) 阻害剤であり、IC50 値は 22 nM、Ki 値は 0.31 nM です 。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 197890-44-1
Sample solution is provided at 25 µL, 10mM.
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GW311616 hydrochloride is a potent, selective, intracellular, orally bioavailable and long duration inhibitor of human neutrophil elastase (HNE) with an IC50 value of 22nM [1].
GW311616 hydrochloride has been found to be selevtive over other human serine proteases with IC50 values of 22nM for HNE, >100μM for trypsin, cathepsin G, and plasmin, >3μM for chymotrypsin and tissue plasminogen activator. In HNE enzyme kinetic tests, GW311616 has been reported to inhibit HNE with a Ki value of 0.13nM. In addition, GW311616 has been revealed to inhibit HWB with an IC50 values of 0.67μM in HWB assay. Moreover, by measurement of intraneutrophil elastase activity, GW311616 hydrochloride has been suggested to have a dose-response and duration of action in blood samples of dog [1].
References:
[1] Macdonald SJ1, Dowle MD, Harrison LA, Shah P, Johnson MR, Inglis GG, Clarke GD, Smith RA, Humphreys D, Molloy CR, Amour A, Dixon M, Murkitt G, Godward RE, Padfield T, Skarzynski T, Singh OM, Kumar KA, Fleetwood G, Hodgson ST, Hardy GW, Finch H. The discovery of a potent, intracellular, orally bioavailable,long duration inhibitor of human neutrophil elastase-GW311616A a development candidate. Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8.
| Cas No. | 197890-44-1 | SDF | |
| 同義語 | GW311616A | ||
| Chemical Name | (3S,3aS,6aR)-3-isopropyl-1-(methylsulfonyl)-4-((E)-4-(piperidin-1-yl)but-2-enoyl)hexahydropyrrolo[3,2-b]pyrrol-2(1H)-one hydrochloride | ||
| Canonical SMILES | CC([C@@](C1=O)([H])[C@@]2([H])[C@@](N1S(C)(=O)=O)([H])CCN2C(/C([H])=C([H])/CN3CCCCC3)=O)C.Cl | ||
| Formula | C19H32ClN3O4S | M.Wt | 433.99 |
| 溶解度 | ≥ 21.7 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3042 mL | 11.521 mL | 23.042 mL |
| 5 mM | 460.8 μL | 2.3042 mL | 4.6084 mL |
| 10 mM | 230.4 μL | 1.1521 mL | 2.3042 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)